PE66798A1 - ANALOGS OF VITAMIN D3 TREATED WITH FLUORINE - Google Patents
ANALOGS OF VITAMIN D3 TREATED WITH FLUORINEInfo
- Publication number
- PE66798A1 PE66798A1 PE1997000387A PE00038797A PE66798A1 PE 66798 A1 PE66798 A1 PE 66798A1 PE 1997000387 A PE1997000387 A PE 1997000387A PE 00038797 A PE00038797 A PE 00038797A PE 66798 A1 PE66798 A1 PE 66798A1
- Authority
- PE
- Peru
- Prior art keywords
- link
- compounds
- carbon
- double
- analogs
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C401/00—Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Nutrition Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIEREN A COMPUESTOS DE FORMULA (I), EN DONDE: "X" ES =CH2 O SON HIDROGENO; R1 Y R2 SON DE PREFERENCIA H, CF3 O CH3, o R1 Y R2 JUNTO CON EL CARBONO 20 FORMAN UN CICLOFLUOROALQUILO O CICLOALQUILO C3-C6, o R1 Y R2 JUNTOS FORMAN =CH2; R3 Y R4 SON DE PREFERENCIA CH3, CF3, CH2CH3, CH2CF3, CF2CH3 Y CF2CF3 o R3 Y R4 JUNTO CON EL CARBONO 25 FORMAN UN CICLOFLUOROALQUILO O CICLOALQUILO C3-C9; "A" ES UN ENLACE SIMPLE O DOBLE; "B" ES UN ENLACE DOBLE O TRIPLE; SIEMPRE QUE: CUANDO "X" ES =CH2, "A" ES UN ENLACE DOBLE, Y: (i) R3 Y R4 SON CF3: SI UNO DE R1 Y R2 ES H, ENTONCES, EL OTRO NO ES CH3; (ii) R3 Y R4 SON ALQUILO C1-C2: SI R2 ES H, ENTONCES, R1 NO ES CH3; (iii) R3 Y R4 SON ALQUILO C1-C4: SI R1 ES H, ENTONCES, R2 NO ES CH3; (iv) R1 ES CH3, R2 ES H: SI UNO DE R3 Y R4 ES CF3, ENTONCES, EL OTRO NO ES CH3; (v) CUANDO "X" SEAN H, R3 Y R4 SON CF3, "A" ES UN ENLACE DOBLE, "B" ES UN ENLACE TRIPLE: SI R2 ES H, ENTONCES, R1 NO ES CH3. TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE LOS COMPUESTOS (I), QUE COMPRENDE ELIMINAR LOS GRUPOS PROTECTORES SILILO; Y A LOS COMPUESTOS INTERMEDIOS DE FORMULA (II), EN DONDE: R1 Y R2 SON CH3 o JUNTO CON EL CARBONO 20 FORMAN UN ANILLO CICLOPROPANO o FORMAN UN =CH2; R3, R4, "A" Y "B" SON COMO SE DEFINIERON PARA (I); "Y" ES H o OSi(CH3)3. LOS COMPUESTOS OBTENIDOS SON USADOS PARA TRATAR LA OSTEOPOROSISTHEY REFER TO COMPOUNDS OF FORMULA (I), WHERE: "X" IS = CH2 OR THEY ARE HYDROGEN; R1 AND R2 ARE OF PREFERENCE H, CF3 OR CH3, or R1 AND R2 TOGETHER WITH CARBON 20 FORM A CYCLOFLUOROALKYL OR CYCLLOALKYL C3-C6, or R1 AND R2 TOGETHER FORMAN = CH2; R3 AND R4 ARE OF PREFERENCE CH3, CF3, CH2CH3, CH2CF3, CF2CH3 AND CF2CF3 or R3 AND R4 TOGETHER WITH CARBON 25 FORM A C3-C9 CYCLOFLUOROALKYL; "A" IS A SINGLE OR DOUBLE LINK; "B" IS A DOUBLE OR TRIPLE LINK; ALWAYS THAT: WHEN "X" IS = CH2, "A" IS A DOUBLE LINK, AND: (i) R3 AND R4 ARE CF3: IF ONE OF R1 AND R2 IS H, THEN THE OTHER IS NOT CH3; (ii) R3 AND R4 ARE C1-C2 ALKYL: IF R2 IS H, THEN, R1 IS NOT CH3; (iii) R3 AND R4 ARE C1-C4 ALKYL: IF R1 IS H, THEN R2 IS NOT CH3; (iv) R1 IS CH3, R2 IS H: IF ONE OF R3 AND R4 IS CF3, THEN THE OTHER IS NOT CH3; (v) WHEN "X" IS H, R3 AND R4 ARE CF3, "A" IS A DOUBLE LINK, "B" IS A TRIPLE LINK: IF R2 IS H, THEN R1 IS NOT CH3. IT ALSO REFERS TO THE PROCEDURE FOR THE PREPARATION OF THE COMPOUNDS (I), WHICH INCLUDES THE ELIMINATION OF THE SILILO PROTECTIVE GROUPS; AND TO THE INTERMEDIATE COMPOUNDS OF FORMULA (II), WHERE: R1 AND R2 ARE CH3 or TOGETHER WITH CARBON 20 FORM A CYCLOPROPAN RING or FORMAN UN = CH2; R3, R4, "A" AND "B" ARE AS DEFINED FOR (I); "Y" IS H or OSi (CH3) 3. THE COMPOUNDS OBTAINED ARE USED TO TREAT OSTEOPOROSIS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1821996P | 1996-05-23 | 1996-05-23 | |
| US3990197P | 1997-03-19 | 1997-03-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE66798A1 true PE66798A1 (en) | 1998-10-22 |
Family
ID=26690870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1997000387A PE66798A1 (en) | 1996-05-23 | 1997-05-16 | ANALOGS OF VITAMIN D3 TREATED WITH FLUORINE |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP0808832B1 (en) |
| JP (1) | JP2859248B2 (en) |
| KR (1) | KR100253961B1 (en) |
| CN (1) | CN100402497C (en) |
| AR (1) | AR007776A1 (en) |
| AT (1) | ATE238278T1 (en) |
| AU (1) | AU733970B2 (en) |
| BR (1) | BR9703385A (en) |
| CA (1) | CA2205315C (en) |
| CO (1) | CO4940503A1 (en) |
| CZ (1) | CZ157797A3 (en) |
| DE (1) | DE69721123T2 (en) |
| DK (1) | DK0808832T3 (en) |
| ES (1) | ES2195049T3 (en) |
| HR (1) | HRP970272A2 (en) |
| HU (1) | HUP9700928A3 (en) |
| IL (1) | IL120844A0 (en) |
| MA (1) | MA24250A1 (en) |
| NO (1) | NO972278L (en) |
| NZ (1) | NZ314840A (en) |
| PE (1) | PE66798A1 (en) |
| PL (1) | PL320130A1 (en) |
| PT (1) | PT808832E (en) |
| SG (1) | SG70010A1 (en) |
| TR (1) | TR199700416A2 (en) |
| YU (1) | YU20097A (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6008209A (en) * | 1997-04-28 | 1999-12-28 | Hoffmann-La Roche Inc. | Method of using vitamin D3 analogs with bis C-20 side chains |
| DE19935771A1 (en) | 1999-07-23 | 2001-02-01 | Schering Ag | New vitamin D derivatives with cyclic substructures in the side chains, processes and intermediates for their manufacture and their use in the manufacture of pharmaceuticals |
| AU2001278744A1 (en) * | 2000-08-17 | 2002-02-25 | Chugai Seiyaku Kabushiki Kaisha | Remedial agent for osteoporosis |
| MXPA04002640A (en) * | 2001-09-21 | 2004-06-07 | Hoffmann La Roche | 3-desoxy-vitamin d3 analog esters. |
| PT103177A (en) | 2003-09-24 | 2005-03-31 | Bioxell Spa | 1-ALPHA-FLUORO-25-HYDROXY-16,23E-DIENE-26,27-BIS-HOMO-20-EPI-COLECALCIFEROL, ITS SALTS OR ESTERS AND ITS USE IN THE MANUFACTURE OF MEDICINES |
| JP2008514621A (en) * | 2004-09-24 | 2008-05-08 | ビオクセル エッセ ピ ア | 20-Cycloalkyl, 26,27-alkyl / haloalkyl-vitamin D3 compounds and methods of use thereof |
| US20090099140A1 (en) * | 2005-03-23 | 2009-04-16 | Bioxell S.P.A. | 20-Alkyl, Gemini Vitamin D3 Compounds and Methods of Use Thereof |
| EP2634171B8 (en) | 2010-10-25 | 2016-01-13 | Teijin Pharma Limited | 23-yne-vitamin d3 derivative |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4141746A1 (en) * | 1991-12-13 | 1993-06-17 | Schering Ag | 20-METHYL-SUBSTITUTED VITAMIN D DERIVATIVES |
| DE4220757A1 (en) * | 1992-06-24 | 1994-01-05 | Schering Ag | Derivatives in the vitamin D series with modifications in the 20-position, process for their preparation, intermediates for this process, pharmaceutical preparations containing these derivatives and their use in the manufacture of medicaments |
| US5428029A (en) * | 1993-11-24 | 1995-06-27 | Hoffmann-La Roche Inc. | Vitamin D3 fluorinated analogs |
| US5384314B1 (en) * | 1994-03-11 | 1997-08-05 | Hoffmann La Roche | 1alpha-fluoro-25-hydroxy-16-ene-23-yne-cholecalciferol |
| WO1997016193A1 (en) * | 1995-10-27 | 1997-05-09 | F. Hoffmann-La Roche Ag | Pharmaceutical composition for treating osteoporosis |
-
1997
- 1997-05-12 SG SG1997001484A patent/SG70010A1/en unknown
- 1997-05-14 ES ES97107868T patent/ES2195049T3/en not_active Expired - Lifetime
- 1997-05-14 EP EP97107868A patent/EP0808832B1/en not_active Expired - Lifetime
- 1997-05-14 PT PT97107868T patent/PT808832E/en unknown
- 1997-05-14 AT AT97107868T patent/ATE238278T1/en not_active IP Right Cessation
- 1997-05-14 DE DE69721123T patent/DE69721123T2/en not_active Expired - Lifetime
- 1997-05-14 CA CA002205315A patent/CA2205315C/en not_active Expired - Fee Related
- 1997-05-14 DK DK97107868T patent/DK0808832T3/en active
- 1997-05-16 IL IL12084497A patent/IL120844A0/en unknown
- 1997-05-16 NZ NZ314840A patent/NZ314840A/en unknown
- 1997-05-16 PE PE1997000387A patent/PE66798A1/en not_active Application Discontinuation
- 1997-05-20 HR HR60/039,901A patent/HRP970272A2/en not_active Application Discontinuation
- 1997-05-20 NO NO972278A patent/NO972278L/en unknown
- 1997-05-20 YU YU20097A patent/YU20097A/en unknown
- 1997-05-21 MA MA24631A patent/MA24250A1/en unknown
- 1997-05-21 AR ARP970102159A patent/AR007776A1/en active IP Right Grant
- 1997-05-21 HU HU9700928A patent/HUP9700928A3/en unknown
- 1997-05-22 CN CNB971134324A patent/CN100402497C/en not_active Expired - Fee Related
- 1997-05-22 KR KR1019970020029A patent/KR100253961B1/en not_active Expired - Fee Related
- 1997-05-22 JP JP9131810A patent/JP2859248B2/en not_active Expired - Fee Related
- 1997-05-22 CZ CZ971577A patent/CZ157797A3/en unknown
- 1997-05-22 CO CO97028096A patent/CO4940503A1/en unknown
- 1997-05-22 PL PL97320130A patent/PL320130A1/en unknown
- 1997-05-22 AU AU23576/97A patent/AU733970B2/en not_active Ceased
- 1997-05-23 BR BR9703385A patent/BR9703385A/en not_active Application Discontinuation
- 1997-05-23 TR TR97/00416A patent/TR199700416A2/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CO4950531A1 (en) | ANALOGS OF VITAMIN D3 PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM | |
| ES2055056T3 (en) | DERIVATIVES OF PIRIMIDOPIRIMIDINA. | |
| ES481220A1 (en) | Novel Aminothiazoles | |
| ES2139943T3 (en) | NEW INHIBITORS OF THE PRINT-GLANDINA SINTASA. | |
| ES2174989T3 (en) | PIRIDO (3,2-E) PIRAZINONAS WITH ANTIASMATICS AND PROCEDURE FOR PREPARATION. | |
| ES2011210T3 (en) | SUBSTITUTED GEM-DIPHOSPHONATE DERIVATIVES, PROCEDURE FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM. | |
| ES2045180T3 (en) | NEW PROCEDURE FOR THE OBTAINING OF 4-ACILOXI-3-HIDROXIETIL-AZETIDINONAS. | |
| ES526318A0 (en) | PROCEDURE FOR THE OBTAINING OF SUBSTITUTED 1-HYDROXYETHYL-TRIAZOLYL DERIVATIVES | |
| AR247402A1 (en) | Improved process for preparing macrolide derivatives | |
| ES2117281T3 (en) | NEW ANALOGS OF VITAMIN D. | |
| PE66798A1 (en) | ANALOGS OF VITAMIN D3 TREATED WITH FLUORINE | |
| AR241593A1 (en) | PROCEDURE FOR PREPARING DERIVATIVES OF QUINOLIN-3-CARBOXYLIC ACID. | |
| AR036000A1 (en) | PROCESS FOR THE PREPARATION OF INDOL DERIVATIVES AND NOVEDOUS INTERMEDIARIES | |
| ES449096A1 (en) | A PROCEDURE FOR THE PREPARATION OF 11-DESOXI-16-ARYLOXI-OMEGA-TETRANORPROSTAGLANDINS. | |
| ES8606382A1 (en) | A PROCEDURE FOR PREPARING A 2'-DESOXI-5-SUBSTITUTED URIDINE DERIVATIVE | |
| ES2145563T3 (en) | NEW IMIDAZOLINE DERIVATIVES WITH AN AFFINITY FOR IMIDAZOLINE RECEPTORS. | |
| DK121383A (en) | PROCEDURE FOR THE PREPARATION OF 8-SUBSTITUTED PYRROLIZIDE INGREDIENTS | |
| SE8003278L (en) | phenylethylamine | |
| PT83452A (en) | Process for preparing alkylmercaptaophenyl-1,3,4-oxa (or thia) iazole derivatives and nematicidal compositions therewith | |
| AR018675A1 (en) | DERIVATIVES OF 3- (2-OXO- [1,3¿I¿] BIPIRROLIDINIL-3-ILIDENOMETIL) -CEFEM, A PHARMACEUTICAL COMPOSITION AND THE USE OF THEM FOR THE MANUFACTURE OF A MEDICINAL PRODUCT. | |
| EA199900460A1 (en) | DERIVATIVES OF BENZULSULPHONE AMID AND MEDICINES CONTAINING MENTIFIED DERIVATIVES | |
| ES464796A1 (en) | PROCEDURE TO PREPARE SUBSTITUTED PHENYLPHOSPHATES. | |
| AU583247B2 (en) | Heteroaryloxypropanolamines | |
| ES520136A0 (en) | A PROCEDURE FOR THE PREPARATION OF A DERIVATIVE OF FURILOXAZOLYL-CETICAL ACID | |
| ES2032461T3 (en) | PROCEDURE FOR PREPARING DERIVATIVES OF INDOL. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |